Articolo in rivista, 2018, ENG, 10.1111/cbdd.13052
Lauria, Antonino; Gentile, Carla; Mingoia, Francesco; Piccionello, Antonio Palumbo; Bartolotta, Roberta; Delisi, Riccardo; Buscemi, Silvestre; Martorana, Annamaria
Univ Palermo; Consiglio Nazl Ric CNR - ISMN
A new series of 3-benzoylamino-5-(1H-imidazol-4-yl)methylaminobenzo[b]furans were synthesized and screened as antitumor agents. As a general trend, tested compounds showed concentration-dependent antiproliferative activity against HeLa and MCF-7 cancer cell lines, exhibiting GI(50) values in the low micromolar range. In most cases, insertion of a methyl substituent on the imidazole moiety improved the antiproliferative activity. Therefore, methyl-imidazolyl-benzo[b]furans compounds were tested in cell cycle perturbation experiments, producing cell cycle arrest with proapoptotic effects. Their core similarity to known colchicine binding site binders led us to further study the structure features as antitubulin agents by in silico protocols.
Chemical biology & drug design (Print) 91 (1), pp. 39–49
3-benzoylamino-5-(1H-imidazol-4-yl)methylaminobenzo[b]furans, antitubulin agents, antitumor agents, colchicine binding site, G2/M phase, HeLa and MCF-7 cell lines, induced fit docking studies, VLAK protocol
ID: 391944
Year: 2018
Type: Articolo in rivista
Creation: 2018-09-27 15:11:41.000
Last update: 2021-04-19 11:41:57.000
CNR authors
External IDs
CNR OAI-PMH: oai:it.cnr:prodotti:391944
DOI: 10.1111/cbdd.13052
ISI Web of Science (WOS): 000418803800004
Scopus: 2-s2.0-85023601315